Zanamivir capsule type inhalation aerosol powder and preparation method thereof

A technology for inhaling powder aerosols and Mivir capsules, which can be used in antiviral agents, pharmaceutical formulations, drug delivery, etc., and can solve the problems of high moisture absorption, poor particle fluidity, content uniformity, emptying rate and low deposition in effective parts and other problems, to achieve the effects of low moisture absorption, good particle fluidity, and simple and easy preparation process

Active Publication Date: 2013-12-11
SHANDONG NEWTIME PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the zanamivir powder aerosol mentioned in this document has poor particle fluidity, high hygroscopicity, and low indicators such as content uniformity, emptying rate and effective part deposition.

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0047] The preparation of embodiment 1 zanamivir inhalation powder

[0048] Zanamivir Superfine Powder 100g

[0049] Ground Lactose 100g

[0050] Crystallized lactose 300g

[0051] A total of 20,000 capsules were made

[0052] Grind the zanamivir raw material, weigh the prescribed amount of zanamivir superfine powder, mix evenly with the prescribed amount of ground lactose, and then mix evenly with the prescribed amount of crystallized lactose, measure the content, calculate the filling amount, and fill it with microcapsules Machine filling in the No. 3 capsule.

[0053] Embodiment 1 sample detection result

[0054] 1. Particle size of dry powder: the particle size of zanamivir is 3.31 μm±0.11 μm.

[0055] 2. Angle of repose: 49°.

[0056] 3. Hygroscopicity: relative weight gain of 2.1%.

[0057] 4. Content uniformity: ±3.0%.

[0058] 5. Empty rate: 99.8%.

[0059] 6. Drug deposition on the effective site: 29%.

[0060] 7. Irritation to respiratory mucosa: no obvious...

Embodiment 2

[0061] The preparation of embodiment 2 zanamivir inhalation powder

[0062] Zanamivir Superfine Powder 100g

[0063] Ground Lactose 200g

[0064] Crystallized lactose 200g

[0065] A total of 20,000 capsules were made

[0066] Grind the zanamivir raw material, weigh the prescribed amount of zanamivir superfine powder, mix evenly with the prescribed amount of ground lactose, and then mix evenly with the prescribed amount of crystallized lactose, measure the content, calculate the filling amount, and fill it with microcapsules Machine filling in the No. 3 capsule.

[0067] Example 2 sample detection result

[0068] 1. Particle size of dry powder: the particle size of zanamivir is 3.67 μm±0.41 μm.

[0069] 2. Angle of repose: 55°.

[0070] 3. Hygroscopicity: relative weight gain of 4.8%.

[0071] 4. Content uniformity: ±3.1%.

[0072] 5. Empty rate: 99.1%.

[0073] 6. Drug deposition on the effective site: 31%.

[0074] 7. Irritation to respiratory mucosa: no obvious ir...

Embodiment 3

[0075] The preparation of embodiment 3 zanamivir inhalation powder spray

[0076] Zanamivir Superfine Powder 100g

[0077] Ground Lactose 40g

[0078] Crystallized lactose 360g

[0079] A total of 20,000 capsules were made

[0080] Grind the zanamivir raw material, weigh the prescribed amount of zanamivir superfine powder, mix evenly with the prescribed amount of ground lactose, and then mix evenly with the prescribed amount of crystallized lactose, measure the content, calculate the filling amount, and fill it with microcapsules Machine filling in the No. 3 capsule.

[0081] Embodiment 3 sample detection result

[0082] 1. Particle size of dry powder: The particle size of zanamivir is 3.97 μm±0.44 μm.

[0083] 2. Angle of repose: 48°.

[0084] 3. Hygroscopicity: relative weight gain of 2.9%.

[0085] 4. Content uniformity: ±3.9%.

[0086] 5. Empty rate: 99.8%.

[0087] 6. The amount of drug deposition on the effective site: 20%.

[0088] 7. Irritation to respiratory...

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Abstract

The invention relates to a zanamivir capsule type inhalation aerosol powder and a preparation method thereof. The capsule type inhalation aerosol powder comprises a capsule shell and a capsule content, wherein the capsule content is composed of 5 parts by weight of zanamivir super micropowder, 10-18 parts by weight of inhalation crystallization lactose and 2-10 parts by weight of inhalation grinding lactose 40M, and average particle size of the zanamivir super micropowder is less than 5mu m and particle size of an excipient is within the range of 40-100mu m. The zanamivir capsule type inhalation aerosol powder provided by the invention has a simple preparation process, good mobility, low hygroscopicity, high content uniformity and high deposit rate on an effective part.

Description

technical field [0001] The invention relates to a medicine for preventing and treating influenza virus, in particular to a zanamivir capsule-type inhalation powder and a preparation method thereof. Background technique [0002] Zanamivir (zanamivir), the chemical name is 5-acetylamino-4-[(aminoiminomethyl)-amino]-2-[(1R,2R)-2,6-anhydro-3,4,5 - Trideoxy-D-glycerol-D-galactosyl-2-enoic acid, an analog of neuraminidase (NA), is a crystal based on the lipid membrane of the virus hemagglutinin and NA Synthesized as a result of X-ray examination of the structure, it is a slow-binding, high-affinity competitive inhibitor of influenza virus NA. Zanamivir can effectively inhibit influenza A and B viruses, and has the same therapeutic effect on many neuraminidase-dependent pathogenic viral epidemics. [0003] Zanamivir has the advantages of high selectivity, low toxicity, strong activity, small dosage, wide range of action, and good preventive effect. However, due to its instabilit...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/72A61K31/351A61P31/16
Inventor 赵志全张丽萍刘阿利
Owner SHANDONG NEWTIME PHARMA
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